Literature DB >> 22505408

Structure of AKR1C3 with 3-phenoxybenzoic acid bound.

Victoria J Jackson1, Yuliana Yosaatmadja, Jack U Flanagan, Christopher J Squire.   

Abstract

Aldo-keto reductase 1C3 (AKR1C3) is a human enzyme that catalyzes the NADPH-dependent reduction of steroids and prostaglandins. AKR1C3 overexpression is associated with the proliferation of hormone-dependent cancers, most notably breast and prostate cancers. Nonsteroidal anti-inflammatory drugs (NSAIDs) and their analogues are well characterized inhibitors of AKR1C3. Here, the X-ray crystal structure of 3-phenoxybenzoic acid in complex with AKR1C3 is presented. This structure provides useful information for the future development of new anticancer agents by structure-guided drug design.
© 2012 International Union of Crystallography. All rights reserved.

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Year:  2012        PMID： 22505408      PMCID： PMC3325808          DOI： 10.1107/S1744309112009049

Source DB:  PubMed          Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun        ISSN： 1744-3091


  24 in total

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Review 8.  Scaling and assessment of data quality.

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Review 2.  AKR1C3 as a target in castrate resistant prostate cancer.

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3.  In situ proteolysis of an N-terminal His tag with thrombin improves the diffraction quality of human aldo-keto reductase 1C3 crystals.

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